3.4.23.45: memapsin 1

This is an abbreviated version!
For detailed information about memapsin 1, go to the full flat file.

Word Map on EC 3.4.23.45

3.4.23.45

alzheimer

abeta

gamma-secretase

aspartyl

amyloid-beta

adam10

alpha-secretase

pharmacology

medicine

tmem27

drug development

Reaction

broad endopeptidase specificity. Cleaves Glu-Val-Asn-Leu-/-Asp-Ala-Glu-Phe in the Swedish variant of Alzheimer's amyloid precursor protein =

Synonyms

aspartic protease BACE2, BACE 2, BACE-1 homologue, BACE-2, BACE2, beta site APP cleaving enzyme, beta-amyloid precursor protein cleavage enzyme 2, beta-secretase, beta-secretase 2, beta-site Alzheimer's amyloid precurser protein cleaving enzyme 2, beta-site amyloid precursor protein cleaving enzyme 2, beta-site amyloid precursor protein-cleaving enzyme 2, beta-site APP cleaving enzyme, beta-site APP cleaving enzyme 2, beta-site APP-cleaving enzyme 2, down region aspartic protease, DRAP, memapsin-1, memapsin1, membrane aspartic protease of the pepsin family, More, protease ASP1, theta-secretase

ECTree

3.4 Acting on peptide bonds (peptidases)

3.4.23 Aspartic endopeptidases

3.4.23.45 memapsin 1

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Results	in table
13	AA Sequence
5	Application
1	CAS Registry Number
16	Cloned(Commentary)
4	Crystallization (Commentary)
252	Disease/ Diagnostics
3	Expression
7	General Information
19	IC50 Value
46	Inhibitors
13	Ki Value [mM]
1	KM Value [mM]
11	Localization
9	Molecular Weight [Da]
35	Natural Substrates/ Products (Substrates)
1	Organic Solvent Stability
47	Organism
31	PDB ID
5	pH Optimum
1	pH Stability
6	Posttranslational Modification
2	Protein Variants
1	Purification (Commentary)
6	Reaction
2	Reaction Type
43	Reference
1	Renatured (Commentary)
72	Source Tissue
1	Specific Activity [micromol/min/mg]
63	Substrates and Products (Substrate)
7	Subunits
53	Synonyms
1	Temperature Optimum [°C]

Inhibitors

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Inhibitors on EC 3.4.23.45 - memapsin 1

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(R)-N-(3-(3-amino-1-methyl-9-oxa-4-thia-2-azaspiro[5.5]undec-2-en-1-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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(R)-N-(3-(3-amino-5-methyl-9,9-dioxido-2,9-dithia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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(R)-N-(3-(3-amino-9,9-difluoro-5-methyl-2-thia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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(R)-N-(3-(7-amino-2,2-difluoro-9-methyl-6-thia-8-azaspiro[3.5]non-7-en-9-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(2,2,2-trifluoroethoxy)pyrazine-2-carboxamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(difluoromethyl)pyrazine-2-carboxamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-chloropicolinamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-fluoropicolinamide

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(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide

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2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole

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inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2

4-[2-(2,6-diethylpyridin-4-yl)-5-(pyrimidin-5-yl)phenyl]-1-methyl-4,5-dihydro-1H-imidazol-2-amine

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6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole

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inhibitor of BACE1, EC 3.4.23.46. 200fold more effective on BACE1 than BACE2

6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole

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inhibitor of BACE1, EC 3.4.23.46. 100fold more effective on BACE1 than BACE2

Asn-Val-Met-Leu-(S)-CH(OH)CH2-Ala-Ala-Ile-Phe

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brefeldin A

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strongly inhibits cleavage of amyloid-beta precursor protein

Cu2+

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70% inhibition at 1 mM

Glu-Glu-Asn-Leu-CH(OH)CH2-Ala-Met-Glu-Phe

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Glu-Val-Asn-Leu-(S)-CH(OH)CH2-Ala-Ala-Glu-Phe

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Glu-Val-Asn-Leu-CONH-Ala-Ala-Glu-Phe

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inhibitors based on this structure, molecular size is substantially reduced while maintaining comparable enzyme inhibitory potencies

Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Stat-Val-Ala-Glu-Phe

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P10-P40 StatVal, beta-secretase inhibitor

N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-5-[methyl(methylsulfonyl)amino]-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N-(3-((4R,5R)-2-amino-5-methoxy-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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N-(3-((4S,5R)-2-amino-4-methyl-5-(tetrahydro-2H-pyran-4-yl)-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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N-(3-((4S,5R)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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N-(3-((4S,5S)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

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N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-methyl-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide

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N-[2-[(4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)pyridine-2-carboxamide

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N-[3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl]-5-chloropyridine-2-carboxamide

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N-[3-[(4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-(1H-1,2,4-triazol-1-yl)pyrazine-2-carboxamide

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N-{(1S,2R)-1-benzyl-2-hydroxy-3-[(3-methylbenzyl)amino]propyl}dibenzo[b,f]oxepine-10-carboxamide

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hydroxyethylamine transition-state inhibitor, binding structure at the active site, interaction mode

N1-((2S,3R)-3-hydroxy-1-phenyl-4-((3-(trifluoromethyl)benzyl)amino)butan-2-yl)-N3,5-dimethyl-N3-((R)-1-phenylethyl)isophthalamide

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N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)pentyl]amino]propyl]-N1-methyl-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide

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N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)propyl]amino]propyl]-5-[methyl(methylsulfonyl)amino]-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide

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Zn2+

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70% inhibition at 1 mM

[(1S,5S,6S)-3-amino-5-(2-fluoro-5-[(Z)-2-fluoro-2-[5-(prop-2-yn-1-yloxy)pyrazin-2-yl]ethenyl]phenyl)-5-methyl-2-thia-4-azabicyclo[4.1.0]hept-3-en-1-yl][(3R)-3-methylmorpholin-4-yl]methanone

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Release 2023.1 (January 2023)